Amidino Hydrazines Or Hydrazones (i.e., N-n=c-n Or N=c-n-n) Patents (Class 514/632)
  • Patent number: 10292950
    Abstract: Disclosed herein are compounds, pharmaceutical compositions, and methods for the treatment of diseases such as inflammation and/or pain, comprising the administration of a therapeutically effective amount of a non-steroidal, non-opioid compound having GI-/renal-/platelet-sparing activities, and wide safety margins with no appreciable inhibition of either form of cyclooxygenase.
    Type: Grant
    Filed: May 12, 2017
    Date of Patent: May 21, 2019
    Assignee: Pathologica LLC
    Inventors: John McKearn, Jeremy Blitzer
  • Patent number: 10080728
    Abstract: The invention relates to medicine, namely, to the solutions used for hemostasis. The hemostatic agent, which represents a polyammonia methanediamine chloride of the general formula where: n=1-20, m=1-10, at that n×m?8. The hemostatic agent may be applied in the form of a 0.01-10% aqueous solution. An aqueous solution of the preparation can be used for impregnation of materials used for bleeding arrest, suture material, bandaging material. The hemostatic agent may be used in the composition of a retraction cord, adhesive pastes, vaginal and rectal suppositories, creams, gels, as well as used with microchips that provide slow release of the preparation. The preparation can also be used in eye drops, eye ointments, and lubricants applied to the surface of the catheter. The drug can be used in endodontic treatment, may be injected into a polymer sealer for root canal obturation, as well as locally—by means of electrophoresis.
    Type: Grant
    Filed: April 20, 2015
    Date of Patent: September 25, 2018
    Inventors: Viktor Veniaminovich Tets, Georgy Viktorovich Tets
  • Patent number: 9775818
    Abstract: The invention comprises methods for treating and preventing a bacterial infection in a subject, methods for preparing a medicament for use in treating and preventing a bacterial infection in a subject, and pharmaceutical and veterinary antibacterial compositions when used therein.
    Type: Grant
    Filed: November 29, 2016
    Date of Patent: October 3, 2017
    Assignee: NEOCULI PTY LTD
    Inventors: Stephen Page, Sanjay Garg
  • Patent number: 9668988
    Abstract: Disclosed herein are controlled-release oral pharmaceutical dosage forms comprising MGBG, and their application for the improved treatment of diseases with reduced side effects and/or longer time at maximum concentration.
    Type: Grant
    Filed: September 9, 2014
    Date of Patent: June 6, 2017
    Assignee: Pathologica LLC
    Inventors: John McKearn, Jeremy Blitzer
  • Patent number: 9616035
    Abstract: Disclosed herein are new oral pharmaceutical compositions of MGBG and related polyamine analogs, polyamine biosynthesis inhibitors, polyamine inhibitors of AMD-I and regulators of osteopontin, and their application for the treatment of disease.
    Type: Grant
    Filed: October 25, 2013
    Date of Patent: April 11, 2017
    Assignee: PATHOLOGICA, LLC
    Inventors: John McKearn, Jeremy Blitzer
  • Patent number: 9539223
    Abstract: The invention comprises methods for treating and preventing a bacterial infection in a subject, methods for preparing a medicament for use in treating and preventing a bacterial infection in a subject, and pharmaceutical and veterinary antibacterial compositions when used therein.
    Type: Grant
    Filed: May 1, 2014
    Date of Patent: January 10, 2017
    Assignee: NEOCULI PTY LTD
    Inventors: Stephen Page, Sanjay Garg
  • Publication number: 20150148359
    Abstract: Uses of a compound of any of Formulas I-VI as a cytotoxic inhibitor of undifferentiated cells are disclosed herein, as well as pharmaceutical compositions comprising a compound of any of Formulas I-VI, and methods for identifying a lead candidate for inhibiting undifferentiated cells. Further disclosed are uses of an SCD-1 inhibitor as a cytotoxic inhibitor of undifferentiated cells.
    Type: Application
    Filed: May 22, 2013
    Publication date: May 28, 2015
    Inventors: Uri Ben-David, Nissim Benvenisty, Payal Arora, Qing-Fen Gan, Ralph J. Garippa
  • Publication number: 20140377345
    Abstract: Disclosed herein are controlled-release oral pharmaceutical dosage forms comprising MGBG, and their application for the improved treatment of diseases with reduced side effects and/or longer time at maximum concentration.
    Type: Application
    Filed: September 9, 2014
    Publication date: December 25, 2014
    Inventors: John McKearn, Jeremy Blitzer
  • Patent number: 8912214
    Abstract: Described herein are Chk2-inhibitor compounds and derivatives thereof, and methods of treating or preventing disease and disease symptoms using the compounds and compositions thereof.
    Type: Grant
    Filed: July 27, 2006
    Date of Patent: December 16, 2014
    Assignee: The United States of America, as Represented by the Secretary, Department of Health and Human Services
    Inventors: Yves Pommier, Robert H. Shoemaker, Dominic Scudiero, Michael Currens, John Cardellina, Andrew Jobson
  • Publication number: 20140364453
    Abstract: A method is disclosed for the in vivo treatment of a breast cancer tumor utilizing a therapeutically effective amount of an agent that inactivates the Rac1 GTPase and results in a reduction in cancer cell invasion, reduced cancer cell motility, and reduced volume and weight of the tumor. Agents that can be used in this treatment include salubrinal, guanabenz, and combinations thereof. The agents additionally have proven useful in reducing the development of osteoclastogenesis and reducing bone metastasis.
    Type: Application
    Filed: June 5, 2014
    Publication date: December 11, 2014
    Applicant: Indiana University Research and Technology Corporation
    Inventors: Hiroki Yokota, Kazunori Hamamura
  • Patent number: 8853276
    Abstract: The invention relates to novel guanidine derivatives in the cinnamic series of general formula (I): The invention also relates to the process for preparing said guanidine derivatives and also to synthetic intermediates. Finally, the invention relates to the use of the guanidine derivatives for the preparation of compositions with anti-glycation properties, especially in cosmetology.
    Type: Grant
    Filed: September 6, 2011
    Date of Patent: October 7, 2014
    Assignee: Produits Chimiques Auxiliaires et de Synthese
    Inventors: Sylvain Rault, Jean Charles Lancelot, Peggy Suzanne, Anne-Sophie Voisin-Chiret, Regis Pecquet, Jean-Christophe Joseph
  • Publication number: 20140235562
    Abstract: A method of treating an ocular disorder in a subject includes administering to the subject a therapeutically effective amount of an agent that modulates at least one target in a signaling cascade associated with light induced retinal degeneration, aberrant all-trans-retinal accumulation, and/or generation of reactive oxygen species (ROS).
    Type: Application
    Filed: April 25, 2014
    Publication date: August 21, 2014
    Inventors: Krzysztof Palczewski, Yu Chen
  • Publication number: 20140187643
    Abstract: Disclosed herein are compounds, pharmaceutical compositions, and methods for the treatment of diseases such as inflammation and/or pain, comprising the administration of a therapeutically effective amount of a non-steroidal, non-opioid compound having GI-/renal-/platelet-sparing activities, and wide safety margins with no appreciable inhibition of either form of cyclooxygenase.
    Type: Application
    Filed: September 23, 2013
    Publication date: July 3, 2014
    Applicant: PATHOLOGICA LLC
    Inventors: John McKearn, Jeremy Blitzer
  • Publication number: 20140051765
    Abstract: Disclosed herein are new oral pharmaceutical compositions of MGBG and related polyamine analogs, polyamine biosynthesis inhibitors, polyamine inhibitors of AMD-I and regulators of osteopontin, and their application for the treatment of disease.
    Type: Application
    Filed: October 25, 2013
    Publication date: February 20, 2014
    Applicant: PATHOLOGICA LLC
    Inventors: John McKearn, Jeremy Blitzer
  • Patent number: 8618091
    Abstract: The present invention provides a photosensitizing composition for treatment of MRSA comprising a photosensitizer and chlorhexidine and a pharmaceutically acceptable carrier. The present invention also provides a method for reducing disease causing microbes comprising: applying the composition comprising a photosensitizer, chlorhexidine at a concentration of more than about 0.01% and less than about 2% v/v, and a pharmaceutically acceptable carrier to a treatment site; and applying light to the treatment site at a wavelength absorbed by the photosensitizer so as to reduce the microbes at the treatment site.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: December 31, 2013
    Assignee: Ondine International Ltd.
    Inventors: Cale Street, Nicolas Loebel, Lisa Pedigo
  • Patent number: 8609734
    Abstract: Disclosed herein are new oral pharmaceutical compositions of MGBG and related polyamine analogs, polyamine biosynthesis inhibitors, polyamine inhibitors of AMD-I and regulators of osteopontin, and their application for the treatment of disease.
    Type: Grant
    Filed: July 24, 2012
    Date of Patent: December 17, 2013
    Assignee: Pathdogica, LLC
    Inventors: John McKearn, Jeremy Blitzer
  • Publication number: 20130317113
    Abstract: The present invention provides methods for the regulation of osteopontin activity in a subject as well as for treating or preventing conditions associated with an increased activity of osteopontin activity in a subject.
    Type: Application
    Filed: April 18, 2013
    Publication date: November 28, 2013
    Applicant: Pathologica LLC
    Inventors: Kenneth G. Hadlock, Hope Lancero, Stephanie Yu, Hien Kim Do
  • Publication number: 20130295009
    Abstract: The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and the pharmacologically active salts thereof;
    Type: Application
    Filed: March 14, 2013
    Publication date: November 7, 2013
    Inventors: Torbjorn LUNDSTEDT, Anna SKOTTNER, Elisabeth SEIFERT
  • Patent number: 8546452
    Abstract: The present invention relates to arylamidrazone derivatives having an antagonistic action against S1P3 receptors represented by the following formula (1) or a pharmaceutically acceptable salt thereof:
    Type: Grant
    Filed: October 11, 2006
    Date of Patent: October 1, 2013
    Assignee: TOA Eiyo Ltd.
    Inventors: Shin-ya Ohnuma, Takeshi Hasegawa, Tomoyuki Sada
  • Patent number: 8497306
    Abstract: The invention relates to pharmaceutically acceptable salts of guanylhydrazone-containing compounds, for example, Semapimod. The invention also relates to pharmaceutically acceptable compositions comprising the salts and methods for their use.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: July 30, 2013
    Assignee: Ferring B.V.
    Inventor: Thais M. Sielecki-Dzurdz
  • Patent number: 8410174
    Abstract: The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and the pharmacologically active salts thereof.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: April 2, 2013
    Assignee: AnaMar AB
    Inventors: Torbjörn Lundstedt, Anna Skottner, Elisabeth Seifert
  • Patent number: 8367645
    Abstract: The invention relates to a composition that includes a first agent selected including an agent that possesses anti-inflammatory activity or acetaminophen, phenacetin, tramadol and the like; a second agent selected from the group consisting of an oxidative phosphorylation inhibitor, an ionophore, and an adenosine 5-monophosphate-activated Protein kinase (AMPK) activator; a third agent that possesses or maintains serotonin activity.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: February 5, 2013
    Inventor: Chien-Hung Chen
  • Publication number: 20120289604
    Abstract: Disclosed herein are new oral pharmaceutical compositions of MGBG and related polyamine analogs, polyamine biosynthesis inhibitors, polyamine inhibitors of AMD-I and regulators of osteopontin, and their application for the treatment of disease.
    Type: Application
    Filed: July 24, 2012
    Publication date: November 15, 2012
    Applicant: PATHOLOGICA LLC
    Inventors: John McKearn, Jeremy Blitzer
  • Patent number: 8309609
    Abstract: The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and the pharmacologically active salts thereof.
    Type: Grant
    Filed: September 28, 2010
    Date of Patent: November 13, 2012
    Assignee: Anamar AB
    Inventors: Torbjörn Lundstedt, Anna Skottner, Elisabeth Seifert
  • Publication number: 20120269891
    Abstract: Disclosed herein are controlled-release oral pharmaceutical dosage forms comprising MGBG, and their application for the improved treatment of diseases with reduced side effects and/or longer time at maximum concentration.
    Type: Application
    Filed: January 19, 2012
    Publication date: October 25, 2012
    Applicant: PATHOLOGICA LLC
    Inventors: John McKearn, Jeremy Blitzer
  • Patent number: 8258186
    Abstract: Disclosed herein are new oral pharmaceutical compositions of MGBG and related polyamine analogs, polyamine biosynthesis inhibitors, polyamine inhibitors of AMD-I and regulators of osteopontin, and their application for the treatment of disease.
    Type: Grant
    Filed: July 16, 2010
    Date of Patent: September 4, 2012
    Assignee: Pathologica, LLC
    Inventors: John McKearn, Jeremy Blitzer
  • Patent number: 8247455
    Abstract: The present invention relates to compounds having the formula: salts thereof; compositions comprising one or more of the compounds and/or salts thereof; methods of using; and methods of making.
    Type: Grant
    Filed: December 7, 2010
    Date of Patent: August 21, 2012
    Assignee: Ferring B.V.
    Inventor: Thais Sielecki-Dzurdz
  • Patent number: 8247406
    Abstract: The present invention provides a photosensitizing composition for treatment of MRSA comprising a photosensitizer and chlorhexidine and a pharmaceutically acceptable carrier. The present invention also provides a method for reducing disease causing microbes comprising: applying the composition comprising a photosensitizer, chlorhexidine at a concentration of more than about 0.01% and less than about 2% v/v, and a pharmaceutically acceptable carrier to a treatment site; and applying light to the treatment site at a wavelength absorbed by the photosensitizer so as to reduce the microbes at the treatment site.
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: August 21, 2012
    Assignee: Ondine International Ltd.
    Inventors: Cale Street, Nicolas Loebel, Lisa Pedigo
  • Publication number: 20120196819
    Abstract: Compositions and methods for the treatment and control of various conditions in an animal which comprises administering to said animal an effective amount of a immediate release composition of about 0.5% to 50% wt/wt of active ingredient together with excipients to a total of about 100%, wherein said compositon dissolves in a relatively short period of time, e.g., 75 seconds or less, 5 seconds or less, or 3 seconds or less, upon administration to said animal.
    Type: Application
    Filed: January 4, 2012
    Publication date: August 2, 2012
    Applicant: NEWMARKET PHARMACEUTICALS LLC
    Inventors: David ROCK, Mark RIDALL
  • Publication number: 20120190751
    Abstract: The present invention relates to the use of benzylideneaminoguanidines for the treatment of inflammation and pain. In one preferred embodiment, the invention relates to the use of N-(2-chloro-3,4-dimethoxybenzylideneamino)guanidine for the treatment of rheumatoid arthritis.
    Type: Application
    Filed: July 30, 2010
    Publication date: July 26, 2012
    Applicant: ANA-MAR AB
    Inventors: Niklas Palmqvist, Anders Sjödin, Christina Wenglén, Christofer Flood, Lennart Lundberg, Elisabeth Seifert, Per Lek, Arne Boman
  • Publication number: 20120178820
    Abstract: The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and the pharmacologically active salts thereof.
    Type: Application
    Filed: March 21, 2012
    Publication date: July 12, 2012
    Applicant: AnaMar AB
    Inventors: Torbjörn LUNDSTEDT, Anna SKOTTNER, Elisabeth SEIFERT
  • Publication number: 20120115959
    Abstract: The present invention relates in general to therapeutic compositions and methods of use. In preferred embodiments, the invention relates to the field of eye health. In some embodiments, the invention relates to the prevention and treatment of macular degeneration by administering compounds disclosed herein. In some embodiments, the invention relates to compositions and methods of improving vision. The present invention includes compositions and methods that provide protection in a patient suffering from an eye disease such as age-related macular degeneration. In certain embodiments, the compositions of the present invention are administered during degeneration, and the composition includes an effective amount of an agent that increases choroidal blood flow.
    Type: Application
    Filed: November 23, 2011
    Publication date: May 10, 2012
    Inventor: George C. Chiou
  • Publication number: 20120108668
    Abstract: The invention relates to the use of endogenous metabolites to produce a metabolic profile of a disorder or disease in a subject, e.g. an autoimmune disease, in particular rheumatoid arthritis, and the analysis of such metabolic profiles in order to find disturbances in such profiles in a subject which are caused by or correlated with the said diseases or disorders. Such disturbances can be normalised by treatment of the subject with specified compounds, particularly N-(2-chloro-3,4-dimethoxybenzylideneamino)guanidine or an aminoguanidine.
    Type: Application
    Filed: March 24, 2010
    Publication date: May 3, 2012
    Inventors: Erik Torbjörn Lundstedt, Nils Johan Trygg, Jon Robert Gabrielsson, Gunilla Ekström, Nils Johan Trygg, Jon Robert Gabrielsson, Gunilla Ekström
  • Patent number: 8148429
    Abstract: The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and the pharmacologically active salts thereof.
    Type: Grant
    Filed: December 15, 2006
    Date of Patent: April 3, 2012
    Assignee: AnaMar AB
    Inventors: Torbjörn Lundstedt, Anna Skottner, Elisabeth Seifert
  • Publication number: 20120022166
    Abstract: Methods for modulating macrophage proliferation in an individual afflicted with or at risk for a macrophage-associated disease are provided. The methods employ a polyamine analog, or salt or protected derivative thereof. Macrophage proliferation has been implicated in a number of serious disorders, including AIDS (HIV)-associated dementia, AIDS-associated non-Hodgkin's lymphoma, and Alzheimer's disease. The invention also provides methods for aiding diagnosis and monitoring therapy of a macrophage-associated non-HIV associated dementia, especially Alzheimer's disease. The invention also provides methods of delaying development of macrophage-associated non-HIV associated dementias, including Alzheimer's disease, which entail administration of an agent which modulates macrophage proliferation.
    Type: Application
    Filed: July 25, 2011
    Publication date: January 26, 2012
    Inventor: Michael S. McGrath
  • Patent number: 8053449
    Abstract: Various methods of administering medication(s) that inhibit the nonenzymatic formation of glycation and dehydration condensation complexes known as advanced glycation end-products (AGEs) or modulate the advanced glycation end-product receptor (RAGE) are provided. Also, a medication releasing medical devices, wherein at least a portion of the medical device releasably includes at least one of these medication(s) are provided.
    Type: Grant
    Filed: October 2, 2006
    Date of Patent: November 8, 2011
    Assignee: Cell Viable Corporation
    Inventor: Jill D. Fabricant
  • Patent number: 8048896
    Abstract: Various methods of administering medication(s) that inhibit the nonenzymatic formation of glycation and dehydration condensation complexes known as advanced glycation end-products (AGEs) or modulate the advanced glycation end-product receptor (RAGE) are provided.
    Type: Grant
    Filed: December 6, 2007
    Date of Patent: November 1, 2011
    Assignee: Cell Viable Corporation
    Inventor: Jill D. Fabricant
  • Publication number: 20110172258
    Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5 and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Application
    Filed: September 22, 2009
    Publication date: July 14, 2011
    Applicant: AQUINOX PHARMACEUTICALS INC.
    Inventors: Jeffery R. Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
  • Publication number: 20110144043
    Abstract: The present invention is directed to methods, kits and compositions for modulating the activity of Stat molecules (e.g., Stat1, Stat3 and Stat5). The compounds of the invention are useful for treating and/or preventing disorders characterized by Stat dysregulation, such as hyperproliferative disorders. Further, the compounds of the present invention are also useful in culturing stem cells and treating ischemic disorders.
    Type: Application
    Filed: December 11, 2009
    Publication date: June 16, 2011
    Applicant: Dana-Farber Cancer Institute
    Inventor: David A. Frank
  • Publication number: 20110112199
    Abstract: Disclosed herein are new oral pharmaceutical compositions of MGBG and related polyamine analogs, polyamine biosynthesis inhibitors, polyamine inhibitors of AMD-I and regulators of osteopontin, and their application for the treatment of disease.
    Type: Application
    Filed: July 16, 2010
    Publication date: May 12, 2011
    Applicant: PATHOLOGICA LLC
    Inventors: John McKearn, Jeremy Blitzer
  • Publication number: 20110091418
    Abstract: Methods for treating viral infections using polyamine analogs, including mitoguazone (MGBG), are provided. In these methods, polyamine analogs destroy macrophages that act as viral reservoirs, facilitating the destruction of the viruses that dwell within the macrophages. Examples of viral infections that may be treated with the present methods include, but are not limited to, infections from human immunodeficiency viruses. These methods differ from previous methods of treatment using polyamine analogs, wherein the polyamine analogs were administered only as anti-tumor agents.
    Type: Application
    Filed: December 21, 2010
    Publication date: April 21, 2011
    Applicant: Pathlogica, LLC
    Inventors: Michael S. McGrath, Kenneth G. Hadlock
  • Patent number: 7879914
    Abstract: Methods for treating viral infections using polyamine analogs, including mitoguazone (MGBG), are provided. In these methods, polyamine analogs destroy macrophages that act as viral reservoirs, facilitating the destruction of the viruses that dwell within the macrophages. Examples of viral infections that may be treated with the present methods include, but are not limited to, infections from human immunodeficiency viruses. These methods differ from previous methods of treatment using polyamine analogs, wherein the polyamine analogs were administered only as anti-tumor agents.
    Type: Grant
    Filed: September 25, 2006
    Date of Patent: February 1, 2011
    Assignee: Pathlogica LLC
    Inventors: Michael S. McGrath, Kenneth G. Hadlock
  • Patent number: 7863334
    Abstract: The present invention relates to compounds having the formula: salts thereof; compositions comprising one or more of the compounds and/or salts thereof; methods of using; and methods of making.
    Type: Grant
    Filed: September 17, 2007
    Date of Patent: January 4, 2011
    Assignee: Cytokine PharmaSciences, Inc.
    Inventor: Thais M. Sielecki-Dzurdz
  • Publication number: 20100285032
    Abstract: ERR? is expressed in bone and cartilage in vivo and osteoblastic and chondrocytic cells in vitro. ERR? is a transcriptional activator of an osteoblast-associated osteopontin (OPN) and chondrocyte-associated (Sox9) gene in osteoblasts and chondrocytes respectively. Knockdown of ERR? expression by antisense oligonucleotide strategies in osteoblastic cell cultures reduces alkaline phosphatase activity. Together these findings indicate that ERR? is expressed in and plays a functional role in bone and cartilage. The results also indicate that agonists and antagonists of ERR? may be useful as therapeutic agents in a wide variety of diseases affecting bones and joints.
    Type: Application
    Filed: June 9, 2008
    Publication date: November 11, 2010
    Inventors: Jane E. Aubin, Marco Cardelli, Ralph A. Zirngibl
  • Publication number: 20100196286
    Abstract: Methods, devices and kits for treating sleep disorders, anxiety disorders, and developmental disorders, and/or for inducing an arousable state of sedation in a subject, are described. For example, inhalation methods, devices and kits for treating insomnia, anxiety and/or ADHD using one or more ?2-adrenergic agonists such as dexmedetomidine or clonidine are described.
    Type: Application
    Filed: December 1, 2009
    Publication date: August 5, 2010
    Inventors: Thomas A. ARMER, Robert O. Cook, Terry Alfredson, Anthony Sun
  • Publication number: 20100179225
    Abstract: A method is provided, comprising administering at least one guanylhydrazone or salt thereof or a combination thereof to a subject to prevent or ameliorate in said subject at least one of postoperative intestinal inflammation, postoperative ileus, ischemia reperfusion injury, or a combination thereof.
    Type: Application
    Filed: September 15, 2009
    Publication date: July 15, 2010
    Applicants: CYTOKINE PHARMASCIENCES, INC., RHEINISCHE FRIEDRICH-WILHELMS-UNIVERSITAT BONN
    Inventors: Jörg KALFF, Sven Wehner, Nico Schäfer, Thais M. Sielecki-Dzurdz
  • Publication number: 20100160332
    Abstract: The adrenergic receptors or adrenoceptors are a family of G-protein coupled receptors split into ? and ? subclasses. The adrenoceptors have important roles in regulating a myriad of physiological conditions and their malfunction has been implicated in the pathophysiology of a number of diseases. Disclosed herein are a series of novel compounds which are ligands of the alpha2-adrenoceptor (?2-ARs) subclass of adrenergic receptors. The invention also provides for pharmaceutical compositions comprising the novel compounds. The compounds are suitable for use in the manufacture of medicaments for the treatment of ?2-ARs associated disorders, such as depression and schizophrenia.
    Type: Application
    Filed: December 22, 2009
    Publication date: June 24, 2010
    Applicant: The Provost, Fellows and Scholars of the College of the Holy and Undivided Trinity of Queen Elizabe
    Inventors: Maria Isabel Rozas Hernando, Fernando Rodriguez Royo
  • Patent number: 7741372
    Abstract: There is disclosed a method for treating diseases and disorders involving T cell activation and HIV-infection using the p38 mitogen activated protein kinase (MAPK) signaling pathway as a target for intervention. There is further disclosed a use for guanylhydrazone-substituted compounds to treat diseases and disorders related to T cell activation and HIV-infection.
    Type: Grant
    Filed: July 16, 2003
    Date of Patent: June 22, 2010
    Assignee: Cytokine PharmaSciences, Inc.
    Inventors: Kevin J. Tracey, Pamela Cohen, Michael Bukrinsky, Helena Schmidtmayerova
  • Publication number: 20100152220
    Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5 and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Application
    Filed: September 22, 2009
    Publication date: June 17, 2010
    Applicant: AQUINOX PHARMACEUTICALS INC.
    Inventors: Jeffery R. Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
  • Publication number: 20100152299
    Abstract: A process for preparing solid dosage forms that contain poorly compressible therapeutic compound. The process, for example, provides for the inventive use of an extruder, especially a twin screw extruder, to melt granulate a therapeutic compound(s) with a granulation excipient.
    Type: Application
    Filed: May 8, 2006
    Publication date: June 17, 2010
    Inventors: Madhav Vasanthavada, Jay Lakshman, Wein-Qin Tong, Abu T. Serajuddin, Yatindra Joshi, James Kowalsi